- Linear and branched alkyl-esters and amides of gallic acid and other (mono-, di- and tri-) hydroxy benzoyl derivatives as promising anti-HCV inhibitors
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Linear and branched compounds that contain two, three or five units of galloyl (3,4,5-trihydroxybenzoyl) or its isomer 2,3,4-trihydroxybenzoyl, as well as other mono- or dihydroxybenzoyl moieties have been synthesized. These molecules have been evaluated for their in vitro inhibitory effects against a wide panel of viruses showing preferential activity against HIV and HCV. Our structure-activity relationship studies demonstrated that the 2,3,4-trihydroxybenzoyl moiety provides better antiviral activities than the galloyl (3,4,5-trihydroxybenzoyl) moiety that is present in natural green tea catechins. This observation can be of interest for the further rational exploration of compounds with anti-HCV/HIV properties. The most notable finding with respect to HIV is that the tripodal compounds 43 and 45, with three 2,3,4-trihydroxybenzoyl moieties, showed higher activities than linear compounds with only one or two. With respect to HCV, the linear compounds, 52 and 41, containing a 12 polymethylene chain and two 2,3 di- or 2,3,4 tri-hydroxybenzoyl groups respectively at the ends of the molecule showed good antiviral efficiency. Furthermore, the anti-HCV activity of both compounds was observed at concentrations well below the cytotoxicity threshold. A representative member of these compounds, 41, showed that the anti-HCV activity was largely independent of the genetic make-up of the HCV subgenomic replicon and cell lines used.
- Rivero-Buceta, Eva,Carrero, Paula,Doyagüez, Elisa G.,Madrona, Andrés,Quesada, Ernesto,Camarasa, María José,Peréz-Pérez, María Jesús,Leyssen, Pieter,Paeshuyse, Jan,Balzarini, Jan,Neyts, Johan,San-Félix, Ana
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p. 656 - 671
(2015/01/30)
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- Synthesis, antibacterial activities and molecular docking studies of peptide and Schiff bases as targeted antibiotics
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A series of peptide and Schiff bases (PSB) were synthesized by reacting salicylic acid, primary diamines with salicylaldehyde or its derivatives, and 40 of which were newly reported. The inhibitory activities against Escherichia coli β-ketoacyl-acyl carrier protein synthase III (ecKAS III) were investigated in vitro and molecular docking simulation also surveyed. Top 10 PSB compounds which posses both good inhibitory activity and well binding affinities were picked out, and their antibacterial activities against Gram-negative and Gram-positive bacterial strains were tested, expecting to exploit potent antibacterial agent with broad-spectrum antibiotics activity. The results demonstrate compound N-(3-(5-bromo-2-hydroxybenzylideneamino)propyl)-2-hydroxybenzamide (2d) can be as a potential antibiotics agent, displaying minimal inhibitory concentration values in the range of 0.39-3.13 μg/mL against various bacteria. Crown Copyright
- Cheng, Kui,Zheng, Qing-Zhong,Qian, Yong,Shi, Lei,Zhao, Jing,Zhu, Hai-Liang
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experimental part
p. 7861 - 7871
(2010/03/24)
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- A Convenient Method for Preparing Some New Macrocyclic Diamides
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A simple and convenient method for preparing macrocyclic diamides containing two sulfur atoms or two to four oxygen atoms of various ring sizes was developed.This two-step procedure is simply composed of reacting salicylic acid or 2-mercaptobenzoic acid w
- Liu, Lilian Kao,Hsieh, Tsing-Pai,Kuo, Sung-Ming
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p. 309 - 312
(2007/10/02)
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- SYNTHESIS OF SOME SALICYLIC ACID DERIVATIVES AND STUDIES OF THEIR INTERACTION WITH URANYL ION
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Some unsubstituted and substituted bis-derivatives of salicylic acid have been synthesized and their acidity constants determined spectrophotometrically in 61.10percent aqueous ethanol.The stability constants of complexes these compounds form with UO2sup
- Djurendic, Evgenija A.,Suranyi, Terezia M.,Miljkovic, Dusan A.
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p. 1446 - 1453
(2007/10/02)
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